The present invention discloses certain derivatives of artemisinin and the active principles contained in Artemisia annua extracts with amino acids, peptides, and amino sugars, and isomers and salts thereof (formula I). The compounds of the present invention possess wide-spectrum antibacterial and antifungal biological activity suitable for topical or oral application for the treatment of infections and topical ailments in mammals, including acne, rosacea, topical wounds, infections, dandruff, skin disfigurements caused by infection, skin discoloration, age spots, wrinkles, excess facial oil, and veterinary problems including canine infections;
                Wherein,        R, together with the interadjacent nitrogen atom, represents an amino acid, amino ester, amino acid amide, peptide, or amino sugar group, and, wherein said amino acid, amino ester, amino acid amide, or peptide is selected from the group consisting of formula (II) and isomers thereof;        
                Wherein,        R1=H, alkyl, aryl, aralkyl, hydroxyalkyl, heterocyclic-alkyl, mercapto-alkyl, dithio-alkyl, carboxyalkyl, amidoalkyl, and guanidinoalkyl;        R2=OR3, NR3R4, and peptide; and        R3, R4=H, alkyl, and aryl; and        n=0 to 10.        
The examples include the compound of formula (III);
and the compound of formula (IV);
and the compound of formula (V);
and the compound of formula (VI);
